title: Monitoring lidocaine single-crystal dissolution by ultraviolet imaging.
abstract: Dissolution critically affects the bioavailability of Biopharmaceutics Classification System class 2 compounds. When unexpected dissolution behaviour occurs, detailed studies using high information content technologies are warranted. In the present study, an evaluation of real-time ultraviolet (UV) imaging for conducting single-crystal dissolution studies was performed. Using lidocaine as a model compound, the aim was to develop a setup capable of monitoring and quantifying the dissolution of lidocaine into a phosphate buffer, pH 7.4, under stagnant conditions. A single crystal of lidocaine was placed in the quartz dissolution cell and UV imaging was performed at 254 nm. Spatially and temporally resolved mapping of lidocaine concentration during the dissolution process was achieved from the recorded images. UV imaging facilitated the monitoring of lidocaine concentrations in the dissolution media adjacent to the single crystals. The concentration maps revealed the effects of natural convection due to density gradients on the dissolution process of lidocaine. UV imaging has great potential for in vitro drug dissolution testing.
authors.affiliation: Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark. Electronic address: joe@farma.ku.dk.
authors.forename: Jesper
authors.initials: J
authors.lastname: Østergaard
authors.affiliation: Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
authors.forename: Fengbin
authors.initials: F
authors.lastname: Ye
authors.affiliation: Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
authors.forename: Jukka
authors.initials: J
authors.lastname: Rantanen
authors.affiliation: Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
authors.forename: Anan
authors.initials: A
authors.lastname: Yaghmur
authors.affiliation: Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
authors.forename: Susan Weng
authors.initials: SW
authors.lastname: Larsen
authors.affiliation: Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
authors.forename: Claus
authors.initials: C
authors.lastname: Larsen
authors.affiliation: Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
authors.forename: Henrik
authors.initials: H
authors.lastname: Jensen
mesh_terms: D003460:Crystallization; D007091:Image Processing, Computer-Assisted; D008012:Lidocaine / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D012995:Solubility; D013499:Surface Properties; D014466:Ultraviolet Rays
chemical_list: D008012:Lidocaine